小叶莲中graphislactone A的分离制备及其抗肿瘤作用机制研究 Preparative isolation of graphislactone A from the fruits of <i>Sinopodophyllum hexandrum</i> and its antitumor action mechanism期刊界 All Journals 搜尽天下杂志传播学术成果专业期刊搜索期刊信息化学术搜索

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小叶莲中graphislactone A的分离制备及其抗肿瘤作用机制研究

引用本文：	高美玲,孙彦君,冯卫生,付露,关延彬,张艳丽,弓建红,陈辉,李晓坤,王彦志.小叶莲中graphislactone A的分离制备及其抗肿瘤作用机制研究[J].中草药,2018,49(1):167-172.

作者姓名：	高美玲孙彦君冯卫生付露关延彬张艳丽弓建红陈辉李晓坤王彦志

作者单位：	河南中医药大学呼吸疾病诊疗与新药研发河南省协同创新中心, 河南郑州 450046;河南中医药大学药学院, 河南郑州 450046,河南中医药大学呼吸疾病诊疗与新药研发河南省协同创新中心, 河南郑州 450046;河南中医药大学药学院, 河南郑州 450046,河南中医药大学呼吸疾病诊疗与新药研发河南省协同创新中心, 河南郑州 450046;河南中医药大学药学院, 河南郑州 450046,河南中医药大学呼吸疾病诊疗与新药研发河南省协同创新中心, 河南郑州 450046;河南中医药大学药学院, 河南郑州 450046,河南中医药大学呼吸疾病诊疗与新药研发河南省协同创新中心, 河南郑州 450046;河南中医药大学药学院, 河南郑州 450046,河南中医药大学呼吸疾病诊疗与新药研发河南省协同创新中心, 河南郑州 450046;河南中医药大学药学院, 河南郑州 450046,河南中医药大学呼吸疾病诊疗与新药研发河南省协同创新中心, 河南郑州 450046;河南中医药大学药学院, 河南郑州 450046,河南中医药大学呼吸疾病诊疗与新药研发河南省协同创新中心, 河南郑州 450046;河南中医药大学药学院, 河南郑州 450046,河南中医药大学呼吸疾病诊疗与新药研发河南省协同创新中心, 河南郑州 450046;河南中医药大学药学院, 河南郑州 450046,河南中医药大学呼吸疾病诊疗与新药研发河南省协同创新中心, 河南郑州 450046;河南中医药大学药学院, 河南郑州 450046

基金项目：	国家自然科学基金资助项目（31300284）；河南中医药大学省属高校基本科研业务专项资金项目（2014KYYWF-QN26）；河南省高等学校青年骨干教师资助计划（2015GGJS-096）；河南中医药大学科技创新人才支持计划（2016XCXRC01）

摘要：	目的确定小叶莲中graphislactone A的制备分离方法;探讨graphislactone A诱导人乳腺癌多药耐药细胞MCF-7/ADR凋亡的作用机制。方法小叶莲药材采用醋酸乙酯超声提取,提取物经过硅胶柱色谱法富集目标成分,再用重结晶法纯化。采用MTT法检测graphislactone A对乳腺癌细胞MCF-7和乳腺癌多药耐药细胞MCF-7/ADR的细胞毒活性。采用流式细胞术、RT-PCR技术和Western blotting法分别检测graphislactone A对乳腺癌多药耐药细胞MCF-7/ADR凋亡、凋亡相关基因及P-糖蛋白(P-gp)蛋白表达的影响。结果建立了小叶莲中graphislactone A的制备分离方法。Graphislactone A对乳腺癌细胞MCF-7和乳腺癌多药耐药细胞MCF-7/ADR具有细胞毒活性,IC50值分别为2.38、9.35μmol/L,且能够上调乳腺癌多药耐药细胞MCF-7/ADR中p53、bax、caspase-3基因的表达,下调bcl-2基因和P-gp的蛋白表达。结论 Graphislactone A为首次从高等植物中发现的酚类化合物,该制备分离方法效率高、样品回收率高,得到的目标成分纯度高。与阳性药依托泊苷相比,Graphislactone A对乳腺癌细胞MCF-7和乳腺癌多药耐药细胞MCF-7/ADR具有较强的细胞毒活性,且能够诱导其凋亡,其机制可能与p53的表达水平上调、激活caspase-3通路、调节bax和bcl-2的相对比例,下调P-gp的蛋白表达有关。
关键词：	小叶莲 graphislactone A 分离制备细胞毒活性多药耐药乳腺癌细胞凋亡
收稿时间：	2017/8/25 0:00:00
*Preparative isolation of graphislactone A from the fruits of Sinopodophyllum hexandrum* and its antitumor action mechanism**

GAO Mei-ling,SUN Yan-jun,FENG Wei-sheng,FU Lu,GUAN Yan-bin,ZHANG Yan-li,GONG Jian-hong,CHEN Hui,LI Xiao-kun and WANG Yan-zhi.Preparative isolation of graphislactone A from the fruits of Sinopodophyllum hexandrum and its antitumor action mechanism[J].Chinese Traditional and Herbal Drugs,2018,49(1):167-172.

Authors:	GAO Mei-ling SUN Yan-jun FENG Wei-sheng FU Lu GUAN Yan-bin ZHANG Yan-li GONG Jian-hong CHEN Hui LI Xiao-kun and WANG Yan-zhi

Institution:	Collaborative Innovation Center for Respiratory Disease Diagnosis and Treatment & amp;Chinese Medicine Development of Henan Province, Henan University of Traditional Chinese Medicine, Zhengzhou 450046, China;School of Pharmacy, Henan University of Traditional Chinese Medicine, Zhengzhou 450046, China,Collaborative Innovation Center for Respiratory Disease Diagnosis and Treatment & amp;Chinese Medicine Development of Henan Province, Henan University of Traditional Chinese Medicine, Zhengzhou 450046, China;School of Pharmacy, Henan University of Traditional Chinese Medicine, Zhengzhou 450046, China,Collaborative Innovation Center for Respiratory Disease Diagnosis and Treatment & amp;Chinese Medicine Development of Henan Province, Henan University of Traditional Chinese Medicine, Zhengzhou 450046, China;School of Pharmacy, Henan University of Traditional Chinese Medicine, Zhengzhou 450046, China,Collaborative Innovation Center for Respiratory Disease Diagnosis and Treatment & amp;Chinese Medicine Development of Henan Province, Henan University of Traditional Chinese Medicine, Zhengzhou 450046, China;School of Pharmacy, Henan University of Traditional Chinese Medicine, Zhengzhou 450046, China,Collaborative Innovation Center for Respiratory Disease Diagnosis and Treatment & amp;Chinese Medicine Development of Henan Province, Henan University of Traditional Chinese Medicine, Zhengzhou 450046, China;School of Pharmacy, Henan University of Traditional Chinese Medicine, Zhengzhou 450046, China,Collaborative Innovation Center for Respiratory Disease Diagnosis and Treatment & amp;Chinese Medicine Development of Henan Province, Henan University of Traditional Chinese Medicine, Zhengzhou 450046, China;School of Pharmacy, Henan University of Traditional Chinese Medicine, Zhengzhou 450046, China,Collaborative Innovation Center for Respiratory Disease Diagnosis and Treatment & amp;Chinese Medicine Development of Henan Province, Henan University of Traditional Chinese Medicine, Zhengzhou 450046, China;School of Pharmacy, Henan University of Traditional Chinese Medicine, Zhengzhou 450046, China,Collaborative Innovation Center for Respiratory Disease Diagnosis and Treatment & amp;Chinese Medicine Development of Henan Province, Henan University of Traditional Chinese Medicine, Zhengzhou 450046, China;School of Pharmacy, Henan University of Traditional Chinese Medicine, Zhengzhou 450046, China,Collaborative Innovation Center for Respiratory Disease Diagnosis and Treatment & amp;Chinese Medicine Development of Henan Province, Henan University of Traditional Chinese Medicine, Zhengzhou 450046, China;School of Pharmacy, Henan University of Traditional Chinese Medicine, Zhengzhou 450046, China and Collaborative Innovation Center for Respiratory Disease Diagnosis and Treatment & amp;Chinese Medicine Development of Henan Province, Henan University of Traditional Chinese Medicine, Zhengzhou 450046, China;School of Pharmacy, Henan University of Traditional Chinese Medicine, Zhengzhou 450046, China

Abstract:

Keywords:	fruits of Sinopodophyllum hexandrum (Royle) Ying graphislactone A isolation and preparation cytotoxic activities multidrug resistance breast cancer cell apoptosis
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